KR920702361A - 10 (1-hydroxyethyl) -11-oxo-1-azatricyclo [7.2.0.0.3.8] undes-2-ene-2-carboxylic acid ester and preparation method thereof - Google Patents

10 (1-hydroxyethyl) -11-oxo-1-azatricyclo [7.2.0.0.3.8] undes-2-ene-2-carboxylic acid ester and preparation method thereof

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Publication number
KR920702361A
KR920702361A KR1019920700916A KR920700916A KR920702361A KR 920702361 A KR920702361 A KR 920702361A KR 1019920700916 A KR1019920700916 A KR 1019920700916A KR 920700916 A KR920700916 A KR 920700916A KR 920702361 A KR920702361 A KR 920702361A
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South Korea
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group
compound
methoxy
alkyl
hydrogen atom
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KR1019920700916A
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Korean (ko)
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KR0169147B1 (en
Inventor
알시드 페르보니
티노 로시
지오반니 가비라기
안토넬라 우르시니
지오르지오 타르지아
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원본미기재
글락소 에스.피.에이.
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Priority claimed from GB909018330A external-priority patent/GB9018330D0/en
Priority claimed from GB919104770A external-priority patent/GB9104770D0/en
Application filed by 원본미기재, 글락소 에스.피.에이. filed Critical 원본미기재
Publication of KR920702361A publication Critical patent/KR920702361A/en
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Publication of KR0169147B1 publication Critical patent/KR0169147B1/en

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D477/00—Heterocyclic compounds containing 1-azabicyclo [3.2.0] heptane ring systems, i.e. compounds containing a ring system of the formula:, e.g. carbapenicillins, thienamycins; Such ring systems being further condensed, e.g. 2,3-condensed with an oxygen-, nitrogen- or sulphur-containing hetero ring
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/04—Antibacterial agents

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Communicable Diseases (AREA)
  • Animal Behavior & Ethology (AREA)
  • Oncology (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Heat Sensitive Colour Forming Recording (AREA)
  • Low-Molecular Organic Synthesis Reactions Using Catalysts (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Plural Heterocyclic Compounds (AREA)

Abstract

내용 없음No content

Description

20(1-히드록시에틸)-11-옥소-1-아자트리시클로[7.2.0.0.3.8]운데스-2-엔-2-카르복실산 에스테르 및 그의 제조 방법20 (1-hydroxyethyl) -11-oxo-1-azatricyclo [7.2.0.0.3.8] undes-2-ene-2-carboxylic acid ester and preparation method thereof

본 내용은 요부공개 건이므로 전문내용을 수록하지 않았음Since this is an open matter, no full text was included.

Claims (13)

하기 일반식(Ⅰ)의 화합물.The compound of the following general formula (I). 상기 식중, R1은기 (상기 식중, R4는 수소 원자 또는 C1-4알킬기를 나타내고; p는 0 또는 1을 나타내고; R5는 C1-4알킬, C1-4알킬기에 의해 치환된 C1-4알킬을 나타냄)를 나타내고, R2는 OR3기(여기서, R3은 C1-4알킬기를 나타냄)를 나타낸다.Wherein R 1 is Group (the above formula, R 4 represents a hydrogen atom or a C 1-4 alkyl group; p is 0 or 1; R 5 is C 1-4 alkyl substituted by C 1-4 alkyl, C 1-4 alkyl group And R 2 represents an OR 3 group, where R 3 represents a C 1-4 alkyl group. 제1항에 있어서, 하기 배위를 가진 화합물.A compound according to claim 1 having the following configuration. 상기 식중, R1및 R2는 제1항에 정의한 바와 같다.In the formula, R 1 and R 2 are as defined in claim 1. 제1항 또는 제2항에 있어서, R4가 수소 원자 또는 메틸기를 나타내는 화합물.The compound of claim 1 or 2, wherein R 4 represents a hydrogen atom or a methyl group. 제1항 내지 제3항중 어느 한항에 있어서, R2가 메톡시 또는 에톡시기를 나타내는 화합물.The compound according to any one of claims 1 to 3, wherein R 2 represents a methoxy or ethoxy group. 제1항 내지 제4항중 어느 한항에 있어서, R5가 메틸, 에틸, 이소프로필, t-부틸, 1-메톡시-1-메틸에틸, 페닐, 시클로헥실 또는 4-에틸시클로헥실기를 나타내는 화합물.The compound according to any one of claims 1 to 4, wherein R 5 represents methyl, ethyl, isopropyl, t-butyl, 1-methoxy-1-methylethyl, phenyl, cyclohexyl or 4-ethylcyclohexyl group. . 제2항에 있어서, R4가 수소 원자 또는 메틸기를 나타내고; R5가 C1-4알킬, C1-2알킬기에 의해 치환될 수 있는 C5-6시클로알킬, 페닐 및 메톡시에 의해 치환된 C1-4알킬로 부터 선택된 기이고; R2가 메톡시기인 화합물.The compound of claim 2, wherein R 4 represents a hydrogen atom or a methyl group; R 5 is C 1-4 alkyl, C 5-6 which may be substituted by a C 1-2 alkyl cycloalkyl, phenyl and methoxy-substituted C 1-4 alkyl, by a group selected from; R 2 is a methoxy group. (4S,8S,9R,10S,12R)-4-메톡시-10-(1-히드록시에틸)-11-옥소-1-아자트리시클로[7.2.0.03,8]운데스-2-엔-2-카르복실산의 피발로일옥시메틸, 1-피발로일옥시에틸, 아세톡시메틸, 1-아세톡시에틸, 1-메톡시-1-메틸에틸카르보닐옥시메틸, 1-(1-메톡시-메틸에틸카르보닐옥시메틸, 1-벤조일옥시에틸, 1-이소프로폭시카르보닐옥시에틸, 시클로헥실옥시카르보닐옥시메틸 및 1-(4-에틸시클로헥실옥시카르보닐옥시)에틸 에스테르.(4S, 8S, 9R, 10S, 12R) -4-methoxy-10- (1-hydroxyethyl) -11-oxo-1-azatricyclo [7.2.0.0 3,8 ] undes-2-ene Pivaloyloxymethyl, 1-pivaloyloxyethyl, acetoxymethyl, 1-acetoxyethyl, 1-methoxy-1-methylethylcarbonyloxymethyl, 2- (1-carboxylic acid Methoxy-methylethylcarbonyloxymethyl, 1-benzoyloxyethyl, 1-isopropoxycarbonyloxyethyl, cyclohexyloxycarbonyloxymethyl and 1- (4-ethylcyclohexyloxycarbonyloxy) ethyl ester. 1-시클로헥실옥시카르보닐옥시메틸 (4S,8S,9R,10S,12R)-4-메톡시-10-(1-히드록시에틸)-11-옥소-1-아자트리시클로[7.2.0.03,8]운데스-2-엔-2-카르복실레이트.1-cyclohexyloxycarbonyloxymethyl (4S, 8S, 9R, 10S, 12R) -4-methoxy-10- (1-hydroxyethyl) -11-oxo-1-azatricyclo [7.2.0.0 3,8 ] undes -2-ene-2-carboxylate. 제1항 내지 제8항중 어느 한항에 있어서, 인간 또는 동물에 있어서 전신 박테리아 감염증의 치료 또는 예방용의 화합물.The compound according to any one of claims 1 to 8, for the treatment or prevention of systemic bacterial infections in humans or animals. 인간 또는 동물 채내에서의 전신 박테리아 감염증의 치료 또는 예방을 위한 치료제의 제조에 있어서의 제1항 내지 제8항중 어느 한항에 정의한 화합물의 용도.Use of a compound as defined in any one of claims 1 to 8 in the manufacture of a therapeutic for the treatment or prevention of systemic bacterial infections in human or animal skin. 1종 이상의 생리학적 허용되는 담체 또는 부형제와 혼합된 제1항 내지 제8항 중 어느 한항에 있어서, 화합물로 이루어진 제약학적 조성물.A pharmaceutical composition according to any one of claims 1 to 8 in admixture with one or more physiologically acceptable carriers or excipients. 제1항 내지 제8항중 어느 한항에 정의된 화합물 유료량을 인간 또는 비인간의 체내에 투여하는 것을 이루어지는 바테리아 감영증을 억제하기 위한 인간 또는 비인간의 치료 방법.A human or non-human treatment method for inhibiting bacterial vaginosis, which comprises administering to the human or non-human body the amount of the compound as defined in any one of claims 1 to 8. (a) 하기 일반식(Ⅱ)의 화합물 또는 그의 염 또는 반응성 유도체를 에스테르화제와 반응시켜 제1항에 정의된 R1기를 도입하거나(a) reacting a compound of formula (II) or a salt or reactive derivative thereof with an esterifying agent to introduce the R 1 group as defined in claim 1 or (상기 식중, R2는 제1항에 정의한 바와 같고, Ra는 수소 원자 또는 히드록시 보호기를 나타냄), 또는 (b)하기 일반식(Ⅲ)의 화합물을 고리화시키고, 그후에 필요 또는 소망에 따라 히드록실 보호기 Ra를 수소 원자에 의해 치환 반응시키고 및(또는) 일반식(Ⅰ)의 화합물의 1종 이상의 다른 이성질체로부터의 그의 특별히 목적하는 이성질체를 분리시키는 것.(Wherein R 2 is as defined in claim 1 and Ra represents a hydrogen atom or a hydroxy protecting group), or (b) cyclizes a compound of the general formula (III) below, and then as required or desired Substituting the hydroxyl protecting group Ra with a hydrogen atom and / or separating its particularly desired isomer from at least one other isomer of the compound of general formula (I). (상기 식중, R1및 R2는 제1항에 정의한 바와 같고, Ra는 수소 원자 또는 히드록실 보호기이고, Y는 산소 원자 또는 포스핀기를 나타냄)으로 이루어지는 제1항에 정의된 일반식(Ⅰ)의 화합물의 제조 방법.(Wherein R 1 and R 2 are as defined in claim 1, Ra is a hydrogen atom or a hydroxyl protecting group, and Y represents an oxygen atom or a phosphine group). Method for preparing a compound of). ※ 참고사항 : 최초출원 내용에 의하여 공개하는 것임.※ Note: The disclosure is based on the initial application.
KR1019920700916A 1990-08-21 1992-04-20 10-(1-hydroxyethyl)-11-oxo-1-azatricyclo(7,2,0,0(3,8))undec-2-ene-2-carboxylic acid esters and a proces for preparing thereof KR0169147B1 (en)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
GB91047704 1990-03-07
GB909018330A GB9018330D0 (en) 1990-08-21 1990-08-21 Heterocyclic compounds
GB90183302 1990-08-21
GB919104770A GB9104770D0 (en) 1991-03-07 1991-03-07 Heterocyclic compounds
PCT/EP1991/001589 WO1992003437A1 (en) 1990-08-21 1991-08-20 10(1-hydroxyethyl)-11-oxo-1-azatricyclo[7.2.0.0.3.8]undec-2-ene-2-carboxylic acid esters and a process for preparing thereof

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KR920702361A true KR920702361A (en) 1992-09-03
KR0169147B1 KR0169147B1 (en) 1999-01-15

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EP (1) EP0495953B1 (en)
JP (2) JP3151215B2 (en)
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CN (1) CN1030917C (en)
AP (1) AP238A (en)
AT (1) ATE106887T1 (en)
AU (1) AU647178B2 (en)
CA (1) CA2067741C (en)
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DK (1) DK0495953T3 (en)
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FI (1) FI97136C (en)
HK (1) HK19495A (en)
HR (1) HRP940556B1 (en)
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MX (1) MX9100743A (en)
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NO (1) NO300176B1 (en)
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OA (1) OA09578A (en)
PL (1) PL169425B1 (en)
PT (1) PT98729B (en)
SG (1) SG169494G (en)
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GB9104838D0 (en) * 1991-03-07 1991-04-17 Glaxo Spa Heterocyclic compounds
AP294A (en) * 1992-08-31 1993-12-28 Glaxo Spa "10-(1-Hydroxyethyl)-11-oxo-1-azatricyclo-(7.2.0.0.3.8) undec-2-ene-2-carboxylic acid derivatives".
GB9218781D0 (en) * 1992-09-04 1992-10-21 Glaxo Spa Heterocyclic derivatives
IN188720B (en) * 1997-11-06 2002-11-02 Panacea Biotec Ltd
JP4377231B2 (en) 2001-11-05 2009-12-02 大日本住友製薬株式会社 New carbapenem compounds
WO2004089954A1 (en) * 2003-04-08 2004-10-21 Sumitomo Pharmaceuticals Co., Ltd. Novel carbapenem compounds
EP1785426A4 (en) * 2004-09-03 2008-02-20 Dainippon Sumitomo Pharma Co Novel carbapenem compound
CA2600374A1 (en) * 2005-03-25 2006-10-05 Dainippon Sumitomo Pharma Co., Ltd. Novel carbapenem compound
EP2085084A1 (en) * 2008-01-29 2009-08-05 LEK Pharmaceuticals D.D. Use of inhibitor of beta-lactamases and its combination with beta-lactam antibiotics
EP2135871A1 (en) * 2008-06-18 2009-12-23 LEK Pharmaceuticals D.D. New trinem antibiotics and inhibitors of beta-lactamases
CA3060396A1 (en) 2017-05-08 2018-11-15 Glaxosmithkline Intellectual Property Development Limited Sanfetrinem or a salt or ester thereof for use in treating mycobacterial infection

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AU636913B2 (en) * 1989-10-11 1993-05-13 Takeda Chemical Industries Ltd. Tricyclic carbapenem compounds
GB9104838D0 (en) * 1991-03-07 1991-04-17 Glaxo Spa Heterocyclic compounds
GB9104832D0 (en) * 1991-03-07 1991-04-17 Glaxo Spa Heterocyclic compounds

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US5587374A (en) 1996-12-24
SG169494G (en) 1995-04-28
JP2000351730A (en) 2000-12-19
PL169425B1 (en) 1996-07-31
HK19495A (en) 1995-02-17
FI921717A (en) 1992-04-16
SK121392A3 (en) 1997-06-04
IE912944A1 (en) 1992-02-26
HUT61024A (en) 1992-11-30
OA09578A (en) 1993-01-31
FI921717A0 (en) 1992-04-16
SI9111427B (en) 2000-10-31
CY2037A (en) 1998-02-20
PT98729A (en) 1992-07-31
IL99248A (en) 1996-01-31
YU142791A (en) 1994-01-20
HRP940556A2 (en) 1996-06-30
ES2054502T3 (en) 1994-08-01
CN1060094A (en) 1992-04-08
AU647178B2 (en) 1994-03-17
NO921521D0 (en) 1992-04-15
EP0495953B1 (en) 1994-06-08
FI97136C (en) 1996-10-25
NZ239474A (en) 1994-06-27
WO1992003437A1 (en) 1992-03-05
DK0495953T3 (en) 1994-07-18
DE69102415D1 (en) 1994-07-14
NO921521L (en) 1992-06-22
CZ121392A3 (en) 1993-04-14
MX9100743A (en) 1992-04-01
FI97136B (en) 1996-07-15
JP3151215B2 (en) 2001-04-03
SK278470B6 (en) 1997-06-04
EP0495953A1 (en) 1992-07-29
HRP940556B1 (en) 2000-06-30
CN1030917C (en) 1996-02-07
MY106997A (en) 1995-08-30
IL99248A0 (en) 1992-07-15
CA2067741C (en) 2002-01-01
CA2067741A1 (en) 1992-02-22
IE66122B1 (en) 1995-12-13
JP3461786B2 (en) 2003-10-27
CZ280942B6 (en) 1996-05-15
KR0169147B1 (en) 1999-01-15
ATE106887T1 (en) 1994-06-15
PT98729B (en) 1999-01-29
AP9100320A0 (en) 1991-10-31
JPH05502044A (en) 1993-04-15
YU48079B (en) 1997-01-08
HU9201303D0 (en) 1992-07-28
AP238A (en) 1993-02-04
HU211584A9 (en) 1995-12-28
NO300176B1 (en) 1997-04-21
AU8421291A (en) 1992-03-17
SI9111427A (en) 1996-12-31
DE69102415T2 (en) 1994-10-13

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